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更新于：2026-04-03
Tirapazamine
替拉扎明
更新于：2026-04-03
概要
基本信息
权益机构- |
最高研发阶段临床3期 |
首次获批日期- |
最高研发阶段(中国)临床2/3期 |
特殊审评孤儿药 (美国)、孤儿药 (欧盟) |
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结构/序列
分子式C7H6N4O2 |
InChIKeyORYDPOVDJJZGHQ-UHFFFAOYSA-N |
CAS号27314-97-2 |
关联
19
项与 替拉扎明 相关的临床试验NCT06844357
A Multi-center, Randomized, Controlled, Open-label Phase II/III Clinical Trial to Investigate Whether Transarterial Tirapazamine Injection Followed by Transarterial Embolization (TATE) is Superior to Traditional Transarterial Chemoembolization (TACE) in Patients With Intermediate-Stage Hepatocellular Carcinoma (HCC)
NCT06848556
A Multicenter, Randomized, Controlled, Open-label Phase I/II Study to Evaluate the Pharmacokinetics of Transarterial Tirapazamine Embolization for Intermediate-stage Hepatocellular Carcinoma, and Compare Its Efficacy and Safety with Transarterial Chemoembolization
NCT03145558
TATE Versus TACE, an Open-label Randomized Study Comparing TransArterial Tirapazamine Embolization Versus TransArterial ChemoEmbolization in Intermediate Stage Hepatocellular Carcinoma
100 项与 替拉扎明 相关的临床结果
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100 项与 替拉扎明 相关的转化医学
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100 项与 替拉扎明 相关的专利（医药）
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638
项与 替拉扎明 相关的文献（医药）2025-10-01JOURNAL OF COLLOID AND INTERFACE SCIENCE
Engineering hypoxia-specific core–shell nanotherapeutics: A sequential strategy for amplified multimodal synergistic breast cancer treatment
Article
作者: Wang, Yuqing ; Qin, Siyong ; Liu, Wenlong ; Liu, Muhai ; Zeng, Fangyu ; Liu, Qiangyu ; Ma, Yihan ; Mo, Qin ; Zhang, Aiqing ; Cheng, Yinjia ; Li, Yuting ; Zhang, Xianzheng
The reactive oxygen species (ROS)-based chemodynamic therapy (CDT) and sonodynamic therapy (SDT) have garnered significant interests in advanced tumor treatments. However, their therapeutic efficacy is severely hindered by tumor hypoxia and overexpressed antioxidant glutathione (GSH) in the tumor microenvironment (TME). Motivated by the concept of metal coordination-based nanomedicine, we proposed an innovative strategy for synergistic tumor therapy tailored to the TME. Herein, we developed a multifunctional targeted delivery nanosystem based on the tirapazamine (TPZ)-loaded BT@M/T@T(Cu)GH cascade nanoreactor to enhance the synergistic efficacy of CDT, SDT, chemotherapy (CT) and starvation therapy (ST) against breast cancer. The rationally designed nanoreactor was constructed through covalent conjugation of glucose oxidase (GOx) onto TPZ-loaded BT@M/T@T(Cu) nanoparticles, wherein the formed tannic acid/copper (Ⅱ) (T(Cu)) network served as the "nanovalve"for BT@M/T nanoparticles. Surface functionalization with hyaluronic acid (HA) enabled BT@M/T@T(Cu) nanoparticles to effectively target CD44-overexpressed 4T1 breast tumors via passive targeting and active targeting effect, while mitigating cytotoxicity toward normal cells/tissues. Following successful tumor accumulation, BT@M/T@T(Cu)GH nanoparticles underwent pH-dependent disassembly and released TPZ, Cu2+ and GOx, initiating a cascade of integrated therapeutic functions, including redox balance disruption, starvation, oxidative cytotoxicity, and hypoxia-activated chemotoxicity. When exposed to ultrasound (US) irradiation, BT@M/T@T(Cu)GH nanoparticles demonstrated sonosensitization capability, generating substantial singlet oxygen (1O2) through energy transfer processes. Owing to all these prominent features, the all-in-one nanomedicine exhibited significant apoptotic cell death and noteworthy tumor eradication in vivo, via synergistic combination of GOx-based ST, self-amplified CDT, hypoxia-activated CT, and US-activated SDT. Additionally, the administration of BT@M/T@T(Cu)GH had negligible effects on the normal growth. Taken together, this work establishes a versatile TiO2-based nanosystem integrating tumor targeting and multi-mode synergistic therapy of breast cancer, offering a novel strategy for highly effective and precise treatment of malignancies.
2025-05-01CHEMICAL ENGINEERING JOURNAL
A vascular heterogeneity-orienting TACE strategy addresses peripheral tumor and avascular deep tumor for complete hepatocellular carcinoma clearance
作者: Yu, Meng ; Li, Shuping ; Tang, Yuhao ; Chen, Jinbin ; Peng, Zhenwei ; Mei, Jie ; Peng, Wei ; Wei, Guangyan ; Zhu, Meiyan ; Xu, Li ; Quan, Xiaolong
Transcatheter arterial chemoembolization (TACE) is considered a frontline therapeutic strategy for intermediate-stage and advanced hepatocellular carcinoma (HCC) through selective embolization of tumor-feeding vessels.However, the exacerbation of hypoxic conditions, along with inefficient drug transport through the bloodstream in residual tumor tissues contributes to poor prognosis after TACE.This study improved the conventional TACE treatment by developing a photothermal-triggered TACE embolization agent (MPMT@Gel), comprising photothermal metal-polyphenol nanocarrier, which loaded with hypoxia-activated chemotherapeutic drug tirapazamine (TPZ) and decorated with penetration enhancer menthol on the surface to serve as photo-controlled release gatekeeper.The MPMT@Gel was activated by near-IR light not only to harness the photothermal-enhanced embolization effect in the xenografted HCC vasculature (p < 0.001), but also to induce the self-feedback cytotoxicity by releasing and distributing the TPZ within hypoxic tumor tissues in response to photothermal stimulation (cell mortality rate of 6.07% to 85.13%).Furthermore, we firstly found that menthol could inhibit tumor angiogenesis (reduced 71.4%) and lung metastasis via reducing EGFR expression (reduced 66.9%).This strategy was demonstrated for the first time on orthotopic HCC mouse model, simultaneously eliminating vascularized peripheral tumor and avascular deep tumor, preventing residual tissue recurrence (HR 0.003; p = 0.004) and lung metastasis (reduced 100%).These findings highlight the great clin. potential of this innovative TACE approach.
2025-05-01Small
Synergistic Comprehensive Activation Methods for Dual‐Modality PDT and Hypoxia‐Triggered Chemotherapy Guided by NIR‐II Imaging beyond 1700 nm in Deep Tumors
Article
作者: Gan, Dechao ; Liu, Shengnan ; Kong, Xianggui ; Li, Dabing ; Li, Qiqing ; Li, Xiaodan ; Chang, Yulei ; Chen, Haoran ; Wang, Wang ; Long, Fei ; Li, Bin
Abstract:
Although photodynamic therapy (PDT) holds great promise for applications in cancer treatment, it has limited effectiveness against deep hypoxic tumors. Moreover, the lack of visualization guidance for precision theranostics poses additional challenges, hindering its broader clinical adoption. By combining NIR‐IIc (1800 nm) imaging guidance with internally and externally activatable dual‐modality PDT and hypoxia‐triggered chemotherapy, this study proposes a conceptual framework to overcome these limitations. This approach involves the use of photoswitchable lanthanide‐doped nanoparticles featuring Tm3+‐activated upconversion/downshifting emissions coupled with carboxyl‐terminated Ir(III) complex‐based Type I/II photosensitizer to form a nanophotosensitizer. The findings demonstrate that this system enabled NIR‐IIc imaging guidance upon 808/980 nm excitation while selectively activating external PDT under 980 nm irradiation, thereby ensuring accurate therapy and minimizing phototoxicity risk. The Ir(III) complex conjugates with luminol to form a self‐illuminating Type I/II photosensitizer, which can respond to the elevated H2O2 levels in the tumor microenvironment, effectively catalyzing chemiluminescence‐assisted PDT. Moreover, PDT aggravates tumor hypoxia, which in turn activates the hypoxia‐activatable prodrugs like tirapazamine, resulting in a synergistic antitumor effect. With NIR‐IIc imaging‐guided dual‐modality PDT, this study introduces a groundbreaking approach that unites Type I/II PDT with chemotherapy, significantly advancing the precise and effective treatment of deep hypoxic tumors.
100 项与 替拉扎明 相关的药物交易
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研发状态
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 肝细胞癌 | 临床3期 | 中国 | 2025-03-11 | |
| 宫颈癌 | 临床3期 | 美国 | 2014-07-28 | |
| 头颈部鳞状细胞癌 | 临床3期 | 美国 | 2005-04-01 | |
| 头颈部鳞状细胞癌 | 临床3期 | 阿根廷 | 2005-04-01 | |
| 头颈部鳞状细胞癌 | 临床3期 | 澳大利亚 | 2005-04-01 | |
| 头颈部鳞状细胞癌 | 临床3期 | 加拿大 | 2005-04-01 | |
| 头颈部鳞状细胞癌 | 临床3期 | 智利 | 2005-04-01 | |
| 头颈部鳞状细胞癌 | 临床3期 | 法国 | 2005-04-01 | |
| 头颈部鳞状细胞癌 | 临床3期 | 德国 | 2005-04-01 | |
| 头颈部鳞状细胞癌 | 临床3期 | 中国香港 | 2005-04-01 |
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临床结果
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适应症
分期
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临床1/2期 | 17 | 夢鑰淵鹹鏇衊遞網構鏇(憲壓簾製艱廠選夢繭窪) = 鹽衊襯製廠夢廠鬱廠鑰 鏇餘選願鬱範衊鑰網觸 (製顧網鏇餘淵簾鬱鑰憲 ) 更多 | 积极 | 2022-06-21 | |||
临床1期 | 27 | 襯齋壓鬱壓醖夢選艱夢(鬱膚鹹顧顧鬱築製鹹製) = hypertension and transient elevation of AST/ALT in 70.4% 選遞夢構齋鏇淵襯觸鏇 (壓襯範鏇糧鏇壓膚艱餘 ) 更多 | 积极 | 2021-05-17 | |||
临床3期 | 402 | (Concurrent Cisplatin and Radiation) | 築淵壓範憲獵鹹積醖膚 = 選淵鹽廠窪網積齋衊顧 築膚鏇顧蓋廠構範夢廠 (夢餘夢齋衊顧憲衊夢憲, 餘顧範鹽餘簾鹽餘網窪 ~ 糧積鏇範醖餘網簾淵製) 更多 | - | 2017-07-02 | ||
(Concurrent Cisplatin, Tirapazamine and Radiation) | 築淵壓範憲獵鹹積醖膚 = 餘壓憲遞鑰網夢醖夢膚 築膚鏇顧蓋廠構範夢廠 (夢餘夢齋衊顧憲衊夢憲, 襯蓋齋鑰製醖範鬱廠艱 ~ 願選衊簾憲願繭夢製鏇) 更多 | ||||||
临床3期 | 861 | 壓積淵衊觸鹽醖鏇積淵(艱製鏇壓獵遞憲窪選築) = 顧襯齋廠積壓廠壓鹹鬱 鏇選範鑰選餘淵襯齋築 (窪製窪遞觸鏇餘夢餘鏇 ) | 不佳 | 2009-11-01 | |||
壓積淵衊觸鹽醖鏇積淵(艱製鏇壓獵遞憲窪選築) = 構鑰襯膚網蓋獵艱壓願 鏇選範鑰選餘淵襯齋築 (窪製窪遞觸鏇餘夢餘鏇 ) | |||||||
N/A | 83 | 鑰鹽蓋鬱壓夢憲糧蓋餘(選繭艱顧醖築鹽簾構廠) = 鬱膚遞簾鏇鑰蓋鹽醖鹽 觸範齋製構鏇範鏇製廠 (窪壓選餘壓積願壓夢糧 ) 更多 | - | 2008-05-20 | |||
临床2期 | 小细胞肺癌 巩固 | 69 | Tirapazamine (TPZ)/cisplatin/etoposide (PE) and concurrent thoracic radiotherapy (TRT) | 襯夢鬱鬱繭壓積窪壓鹹(艱鹹淵醖願觸齋糧獵鑰) = 鬱築膚積鏇構衊繭窪願 獵襯艱顧選壓廠糧顧顧 (觸簾鏇廠獵齋獵築鹽淵 ) 更多 | - | 2008-05-20 | |
临床1期 | 11 | 蓋艱遞蓋糧遞繭築積鑰(壓衊夢製夢繭顧製鏇獵) = 鑰艱夢繭積憲鹹築齋選 膚膚鬱繭淵選網鹽廠築 (選憲齋膚繭醖鑰獵鑰糧 ) 更多 | - | 2007-06-20 | |||
临床2期 | 63 | TPZ arm | 遞網範廠夢簾製憲網艱(鹽築鑰積繭鹹鏇膚築獵) = 夢範範製鹹範夢淵網鹹 範積製構選廠艱齋窪積 (積膚鑰願齋餘艱築夢蓋 ) 更多 | - | 2006-05-01 | ||
临床2期 | 65 | 簾廠鬱積衊艱齋願製夢(艱願鏇鹹簾齋製餘遞壓) = frequent constitutional (23%) grade 3 or 4 toxicity 糧艱窪範齋積膚窪網遞 (選簾廠觸繭艱簾壓鏇鹹 ) 更多 | 积极 | 2006-03-01 | |||
N/A | 56 | 餘憲積廠餘蓋顧憲鬱鏇(糧獵顧膚膚艱糧願選齋) = three cases 遞範觸鹹觸繭鬱膚夢網 (鬱蓋積淵鑰鹹夢憲願壓 ) 更多 | - | 2006-01-01 |
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